Skeletal accumulation of bisphosphonates: implications for osteoporosis treatment.
BACKGROUND
Bisphosphonates (BPs), the gold-standard pharmacological treatment for osteoporosis, are unique in that they become physically bound to the bone matrix and therefore accumulate over time. This skeletal accumulation has important physiological implications that are not completely understood.


OBJECTIVE
To review concepts related to the biological effects of BP accumulation in the skeleton.


METHODS
Articles concerning skeletal accumulation of BP treatment were identified.


CONCLUSIONS
Skeletal accumulation of BP, dictated by both chemical and biological factors, is dose-dependent, differs among skeletal sites and likely differs among the various BPs. Bisphosphonate embedded within the skeletal matrix has lasting biological effects, the results of which have both positive and negative implications for bone remodeling. As alternative anti-remodeling agents gain approval for treatment of osteoporosis, the property of skeletal accumulation will likely be unique to BPs and therefore may be the property that determines the future use of this drug class.
Allen
Matthew R
MR
Indiana University School of Medicine, Department of Anatomy & Cell Biology, 635 Barnhill Drive, MS-5035, IN 46202, Indianapolis, USA. matallen@iupui.edu
D000818:Animals; D050071:Bone Density Conservation Agents / Q000009:adverse effects* / Q000737:chemistry / Q000378:metabolism* / Q000627:therapeutic use; D016723:Bone Remodeling / Q000187:drug effects; D001842:Bone and Bones / Q000378:metabolism*; D003599:Cytoskeleton / Q000378:metabolism; D004164:Diphosphonates / Q000009:adverse effects* / Q000737:chemistry / Q000378:metabolism* / Q000627:therapeutic use; D006801:Humans; D007568:Jaw / Q000473:pathology; D010020:Osteonecrosis / Q000139:chemically induced / Q000473:pathology; D010024:Osteoporosis / Q000188:drug therapy* / Q000378:metabolism*
D050071:Bone Density Conservation Agents; D004164:Diphosphonates